Method for increasing the bioavailability of glycopyrrolate
View Patent ↗The invention relates to a method of treating sialorrhea in a human patient, which comprises orally administering glycopyrrolate in a liquid solution to the human patient under fasted conditions.
1. A method of treating sialorrhea in a human patient, which comprises orally administering about 1 mg to about 10 mg of glycopyrrolate in a liquid solution to the human patient under fasted conditions, wherein the ratio of the extent of absorption of glycopyrrolate at t=∞ (AUC 0-∞ ) following administration without food to AUC 0-∞ following administration with food is greater than 1.8, and wherein the patient has not consumed food during the period from 30 minutes prior to the administration of glycopyrrolate to 1 hour after the administration of glycopyrrolate.
2. The method of claim 1 , wherein the AUC 0-∞ following administration under fasted conditions is greater than 1.0 ng*hr/mL.
3. The method of claim 1 , wherein the AUC 0-∞ following administration under fasted conditions is greater than 1.7 ng*hr/mL.
4. A method of treating sialorrhea in a human patient, which comprises orally administering about 1 mg to about 10 mg of glycopyrrolate in a liquid solution to the human patient under fasted conditions,
wherein the administration of glycopyrrolate under fasted conditions results in an increase of the maximum plasma concentration (C max ) and the extent of absorption of glycopyrrolate at t=24 hours (AUC 0-24 hrs ) as compared to the administration of glycopyrrolate under fed conditions,
wherein the ratio of C max following administration without food to C max following administration with food is greater than 1.1,
wherein the ratio of AUC 0-24 hrs following administration without food to AUC 0-24 hrs following administration with food is greater than 1.8,
wherein the AUC 0-24 hrs following administration under fasted conditions is greater than 1.0 ng*hr/mL, and
wherein the patient has not consumed food during the period from 30 minutes prior to the administration of glycopyrrolate to 1 hour after the administration of glycopyrrolate.
5. The method of claim 4 , wherein the AUC 0-24 hrs following administration under fasted conditions is greater than 1.7 ng*hr/mL.
6. The method of claim 4 , wherein the ratio of the extent of absorption of glycopyrrolate at t=∞ (AUC 0-∞ ) following administration without food to AUC 0-∞ following administration with food is greater than 1.8.
7. The method of claim 6 , wherein the extent of absorption of glycopyrrolate at t=∞ (AUC 0-∞ ) following administration under fasted conditions is greater than 1.0 ng*hr/mL.
8. The method of claim 7 , wherein the AUC 0-∞ following administration under fasted conditions is greater than 1.7 ng*hr/mL.